LPL Receptor Agonist

GRI977143 is a specific LPA₂ receptor agonist, with an EC₅₀ of 3.3 μM .

CYM50260 is a potent and exquisitely selective sphingosine-1-phosphate 4 receptor (S1P₄-R) agonist with an EC₅₀ of 45 nM. CYM50260 displays no activity against S1P₁-R, S1P₂-R, S1P₃-R and S1P₅-R.

Radioprotectin-1 is a potent and specific nonlipid agonist of lysophosphatidic acid receptor 2 (LPA₂), with an EC₅₀ value of 25 nM for murine LPA₂ subtype.

Ceralifimod (ONO-4641) is selective, high potent agonist for sphingosine 1-phosphate receptors 1 and 5, with EC₅₀s of 27.3, 334 pM for human S1P receptor 1 and 5, respectively.

Sphingosine-1-phosphate-d₇ is the deuterium labeled Sphingosine-1-phosphate. Sphingosine-1-phosphate (S1P) is an agonist of S1P1-5 receptors and a ligand of GPR3, GPR6 and GPR12.?Sphingosine-1-phosphate is an intracellular second messenger and mobilizes Ca2+ as an extracellular ligand for G protein-coupled receptors. Sphingosine-1-phosphate is an important lipid mediator generated from Sphingomyelin (HY-113498) or other membrane phospholipids.

A-971432 is a potent, selective and orally active sphingosine-1-phosphate (S1P) receptor 5 agonist with IC₅₀s of .362, >10, 0.006 μM for S1P1, S1P3, S1P5 respectively. A-971432 protects blood–brain barrier (BBB) homeostasis. A-971432 reverses age-related cognitive decline. A-971432 has the potential for the research of alzheimer’s disease or multiple sclerosis .

CYM50179 (compound 22n) is a potent and selective S1P4-R (Sphingosine-1-phosphate4 receptor) agonist with an EC₅₀ of 46 nM.

RP-001 hydrochloride is a picomolar short-acting S1P1 (EDG1) selective agonist, with an EC₅₀ of 9 pM. RP-00 hydrochloride induces internalization and polyubiquitination of S1P1. RP-001 hydrochloride has little activity on S1P2-S1P4 and only moderate affinity for S1P5.

GSK2018682 is an agonist for S1P1 and S1P5 receptor with pEC₅₀s of 7.7 and 7.2, respectively, and has no agonist activity towards human S1P2, S1P3, or S1P4. GSK2018682 is used in the research of multiple sclerosis.

NAEPA, a phosphate-mimetic derivative, is a lysophosphatidic acid (LPA) receptor agonist.

ASP-4058 is a next-generation, selective and oral bioactive agonist for Sphingosine 1-Phosphate receptors 1 and 5 (S1P₁ and S1P₅), ameliorates rodent experimental autoimmune encephalomyelitis with a favorable safety profile.

Siponimod (BAF-312) hemifumarate is an orally active, blood-brain barrier penetrant dual agonist of S1P1/S1P5, with EC₅₀ values of 0.39 nM and 0.98 nM, respectively. Siponimod hemifumarate induces S1P1 internalization, activates GIRK channels, inhibits lymphocyte egress, reduces peripheral lymphocyte counts, triggers transient bradycardia, prevents synaptic neurodegeneration, promotes remyelination, alleviates demyelination, and prevents the loss of GABAergic interneurons. Siponimod hemifumarate can be used in research related to multiple sclerosis.

TRV045 is a selective Sphingosine-1-phosphate subtype 1 receptor agonist with no effect on lymphocyte transport. TRV045 has antiepileptic activity.

RP101075, an active metabolite of Ozanimod, is a potent, orally active S1PR (sphingosine-1-phosphate receptor 1) agonist, with an EC₅₀ of 0.27 nM. RP101075 displays >100-fold selectivity over S1PR5 (EC₅₀=5.9 nM) and >10000-fold over S1PR 2, 3, and 4. RP101075 displays superior cardiovascular safety profile.

IMMH001, also called SYL930, is an orally active, potent and selective S1P1 (sphingosine-1-phosphate receptor 1) agonist. IMMH001 decreased levels of both chemokines and proinflammatory cytokines, including IL-1β, IL-5, IL-18, IP10, CCL3, and CCL5. IMMH001 can be used for rheumatoid arthritis (RA) research.

S1P1 Agonist 1 is a S1P1 agonist with immunomodulatory activities.

L-threo Lysosphingomyelin (d18:1) (L-threo-Sphingosylphosphorylcholine) is an endogenous bioactive sphingolipid. L-threo Lysosphingomyelin (d18:1) is a potent S1P receptor agonist with EC₅₀s of 19.3, 131.8, and 313.3 nM for hS1P₁, hS1P₃, and hS1P₂, respectively.

CYM-5482 is a potent and selective agonist Sphingosine 1-phosphate receptor 2 (S1PR2) with an IC₅₀ and EC₅₀ of 1.0 and 1.03 μM. CYM-5482 has the potential for the research of cancer diseases.

UCM-05194 (ammonium) is a lysophosphatidic acid receptor 1 (LPA1) agonist. UCM-05194 (ammonium) induces calcium mobilization in LPA1-expressing RH7777 cells (EC₅₀ = 0.24 µM). UCM-05194 (ammonium) induces neurite retraction and migration in LPA1-overexpressing B103 rat neuroblastoma cells. UCM-05194 (ammonium) attenuates acetic acid-induced writhing and hind paw mechanical hypersensitivity in mice.

Ponesimod-d₄ (ACT-128800-d₄) is the deuterium labeled Ponesimod (HY-10569). Ponesimod (ACT-128800) is a potent, selective and orally active agonist of S1P₁, with an IC₅₀ of 6 nM in a radioligand binding assay. Ponesimod activates S1P₁-mediated signal transduction with high potency (EC₅₀=5.7 nM). Ponesimod can protect against lymphocyte-mediated tissue inflammation.